TECHNICAL PROGRAM - American Chemical Society Publications

455. Solid phase synthesis of dendritic prodrugs
of salicylic acid. D. Cater, M. Chai,
G. Lu
456. Synthesis of water-soluble salicylic acid
analogs by sugar-conjugation.
D. MacHue, J. Rowlett, M. Chai
457. Improved synthesis of the epoxy isoprostane
phospholipid PEIPC and its analogs.
W. Zhong, J. Springstead,
J. A. Berliner, M. E. Jung
458. Design and synthesis of new derivatives
of YK-4-279 as inhibitors of EWS-FLI1.
P. N. Tosso, L. Jacobwitz, J. A. Toretsky,
M. L. Brown, Y. Kong
459. Design and synthesis of homodinuclear
cyclen-based SH2 domain proteomimetics.
S. Haftchenary,
S. Fletcher, J. A. Drewry, J. Turkson,
P. T. Gunning*
460. Discovery of potent and selective inhibitors
for ADAMTS-4 through encoded library
technology (ELT). Y. Ding,
H. O’Keefe, J. L. Svendsen,
G. J. Franklin, P. A. Centrella, M. A. Clark,
R. A. Acharya, F. Li, J. A. Messer,
C. H. Chiu, R. E. Matico,
M. F. Murray-Thompson, S. R. Skinner,
S. L. Belyanskaya, D. I. Israel,
J. W. Cuozzo, C. C. Arico-Muendel,
B. A. Morgan
461. Novel chemical probes for p300 HAT inhibition.
C. Mukherjee, D. J. Meyers,
E. M. Bowers, P. A. Cole
462. Studies of ciprofloxacin encapsulation
on biogels in organic solvent mixtures.
V. E. Bosio, G. A. Islan, D. Kaplan,
G. R. Castro
463. New and efficient synthesis of regiospecifically
deuterated covalent probes for
cannabinoid receptors. G. A. Thakur,
R. Sharma, A. Makriyannis
464. Design and synthesis of a biotinylated
derivative of the tylophorine analog DCB-
3503. S. Francis, D. C. Baker,
J. Gutierrez, Y. Cheng, X. Wang
465. Optimization of alkyl amine renin inhibitors.
C. M. Tice, R. D. Simpson, J. Yuan,
Z. Xu, W. Zhao, L. Jia, S. Cacatian,
P. T. Flaherty, J. Guo, A. Ishchenko,
S. B. Singh, Z. Wu, B. M. McKeever,
B. B. Scott, Y. Bukhtiyarov, J. Berbaum,
R. Panemangalore, C. P. Doe,
R. N. Willette, R. K. Harrison,
G. M. McGeehan, L. W. Dillard,
J. J. Baldwin, D. A. Claremon
466. Effects of lead and mercury on the
blood proteome of children.
K. Bendinskas, R. Birdsall, M. Kiley,
J. A. MacKenzie
467. Helping build better pre-clinical drug
candidates: Pharmaceutical development
programs at the discovery-development
interface. J. D. Higgins, A. Templeton,
E. Kwong
468. Correlative microscopy: Concurrent
SEM and optical imaging of cells in an
open system. D. Guarrera, H. Nishiyama,
M. Suga, C. Sato
469. Active targeting with controlled delivery
of therapeutic agents to bone using versatile,
bifunctional bisphosphonates.
J. Yewle, D. Puleo, L. Bachas
470. Design and synthesis of Mycobacterial
proteasome inhibitors. G. V. Clements,
H. I. Boshoff, C. S. Dowd
471. New and facile way to Flustramine analogs
through radical cyclization.
G. A. Kraus, J. Beasley
472. Fundamental oxidation and reduction
chemistry of isoniazid and its reactive intermediates.
K. A. Rickman, S. P. Mezyk,
J. J. Kiddle
473. Capture compound mass spectrometry:
A novel chemical proteomics approach to
profile small molecule-protein interactions
for drug target discovery and offtarget
binding-induced toxicity.
M. Sefkow, S. Michaelis, C. Dalhoff,
J. J. Fischer, O. Y. Graebner, F. Kroll,
M. Glinski, M. Dreger, H. Koester
474. Pyrrolopyrimidine-based P2X3 antagonists
for the treatment of pain. L. Cantin,
M. Bayrakdarian, C. Buon, Y. Hu,
V. Kennedy, M. Laplante, C. Leung,
X. Luo, N. Popovic, O. René,
V. Santhakumar, J. Butterworth,
C. Godbout, M. Gosselin, E. Grazzini,
J. Labrecque, M. Paré, D. Projean,
X. Hong Yu, M. J. Tomaszewski
475. Drug discovery: Natural herbal formulation.
J. L. Chan
476. Synthesis and preliminary biological
evaluation of 20-epi-eldecalcitol [20-Epi-
1alfa,25-dihydroxy-2beta-(3-hydroxypropoxy)vitamin
D3: 20-Epi-ED-71].
S. Hatakeyama, M. Yoshino, K. Eto,
K. Takahashi, J. Ishihara, Y. Ono,
H. Saito, N. Kubodera
477. Investigation of preparative HPLC applications
performed at both acidic and basic
pH. J. W. Benedict
478. Novel lacZ responsive enhanced Gdbased
1 H MRI agents. J. Yu,
J. Magnusson, R. P. Mason
479. Synthesis of tetralene- and chromenebased
4EGI-1 mimetics as inhibitors of
eIF4E/eIF4G interaction. P. Mahalingam,
Y. Wang, L. Chen, N. Zhang, J. J. Levy,
E. Papadopoulos, B. H. Aktas,
G. Wagner, J. A. Halperin, M. Chorev
480. Spiro-benzamides as ENT-1 inhibitors.
D. Berthelot, S. Pieters, M. De Cleyn,
J. Bosmans, S. Pype, T. Meert
481. Depth dependent swelling and mechanical
behavior of cartilage. F. Horkay,
I. Horkayne-Szakaly, E. K. Dimitriadis,
C. Silva, P. J. Basser
482. Evaluation of select fractions of mineral
oil in vaccine preparation. R. S. Stahl,
J. M. kemp, L. A. Miller
483. Loading the dice by integrating lead optimization.
R. D. Clark, D. Miller,
R. Fraczkiewicz, M. Waldman,
M. B. Bolger, W. S. Woltosz
484. Withdrawn
THURSDAY MORNING
Section A
Boston Convention & Exhibition Center
Room 259A/B
General Oral Session
J. Zablocki, Organizer
X. Wang, Presiding
8:30 485. Multicomponent reactions for the
discovery of p53-Mdm2 antagonists:
Synthesis, chemoinformatics and biological
evaluations. Y. Huang,A.Dömling
8:50 486. Discovery of novel macrolide antibiotics:
Synthesis and biological evaluation
of 4,8,10-tridesmethyl telithromycin.
V. Velvadapu, T. Paul, B. S. Wagh,
R. B. Andrade
9:10 487. Engineered immunity: Development
of multivalent artificial opsonins for
the treatment of nosocomial infections.
K. N. Katzenmeyer, J. D. Bryers
9:30 488. Identification and SAR of novel furan-free
imidazopyridine ligands as selective
adenosine A2A-antagonists for Parkinson
disease. S. Schann, S. Mayer,
L. Cardona, S. Gardan, N. Hubert,
A. Haberkorn, E. Steinberg, L. Baron,
C. Franchet, P. Neuville
9:50 489. Discovery of BKM120, a pan class
I PI3 kinase inhibitor in phase I/II clinical
trials. M. T. Burger, S. Pecchi,
A. Wagman, Z. Ni, M. Knapp, G. Atallah,
K. Pfister, S. Ng, A. Smith, T. Pick,
K. Frazier, J. Verhagen, Y. Zhang,
S. Bartulis, T. Hendricksen, E. Iwanowicz,
J. Hazenadar, K. Huh, A. Ashash, X. Xin,
D. Menezes, H. Merritt, M. Wiesmann,
C. Voliva
10:10 490. Design and synthesis of dual
adenosine A 2A/A 1 antagonists for the
treatment of Parkinson’s disease.
B. C. Shook
10:30 491. Synthesis and biological activity
of 2H-quinolizin-2-one based p38-a MAP
kinase inhibitors. R. M. Tynebor,
M. Chen, S. R. Natarajan, E. A. O’Neill,
J. E. Thompson, C. E. Fitzgerald,
S. J. O’Keefe, J. B. Doherty
10:50 492. Evaluation of 4-cyano-4-arylpiperidine
quinolizidinone carboxylic acid
selective M 1 positive allosteric receptor
modulators. S. D. Kuduk,R.K.Chang,
C. N. Di Marco, D. R. Pitts, W. J. Ray,
L. Ma, M. Wittmann, M. A. Seager,
K. A. Koeplinger, C. D. Thompson,
G. D. Hartman, M. T. Bilodeau
11:10 493. Discovery of the potent PI3K/
mTOR dual inhibitor PF-04979064.
H. Cheng, S. Bagrodia, S. Bailey,
S. M. Baxi, L. Goulet, L. Guo, J. Hoffman,
T. O. Johnson, T. W. Johnson, C. Li, J. Li,
K. Liu, Z. Liu, M. A. Marx, G. Paderes,
S. Sun, M. Walls, P. A. Wells, A. Yang,
M. Yin, J. Zhu
11:30 494. Identification of PKI-179 as a potent
and orally efficacious PI3 kinase inhibitor
for the treatment of cancer.
Z. Chen, A. M. Venkatesan
11:50 495. Design and synthesis of tricyclic
sulfones as g-secretase inhibitors with
greatly reduced Notch toxicity. R. Xu,
D. Cole, T. Asberom, T. Bara, C. Bennett,
D. A. Burnett, J. Clader, M. Domalski,
W. Greenlee, L. Hyde, H. Josien, H. Li,
M. McBriar, B. McKittrick, A. T. McPhail,
D. Pissarnitski, L. Qiang, M. Rajagopalan,
T. Sasikumar, J. Su, H. Tang, W. Wu,
L. Zhang, Z. Zhao
12:10 496. Discovery of PPIs using chemical
feature-based pharmacophore models.
T. Langer
Section B
Boston Convention & Exhibition Center
Room 253A/B
Pharmacological Manipulation of
Endocannabinoid Degradation
J. Breitenbucher, S. McAlpine, Organizers,
Presiding
8:30 Introductory Remarks
8:40 497. Targeting endogenous cannabinoid
catabolic enzymes in preclinical
models of pain. A. H. Lichtman
9:20 498. Discovery of a novel series of potent,
non-covalent fatty acid amide hydrolase
(FAAH) inhibitors through rational
design. D. J. Gustin,Z.Ma,Y.Li,
C. Hedberg, X. Min, C. Guimaraes,
Z. Wang, N. Walker, M. Lindstrom,
R. Connors, A. C. Porter,
D. Lester-Zeiner, F. Kayser
10:00 499. Inhibitors of fatty acid amide hydrolase
(FAAH): SAR and results in preclinical
pain models. M. S. Tichenor,
J. M. Keith, R. L. Apodaca, W. Xiao,
W. Jones, A. L. Chambers, M. Seierstad,
J. Pierce, J. A. Palmer, M. Webb,
M. J. Karbarz, L. Chang, S. J. Wilson,
L. Luo, M. L. Wennerholm, S. M. Brown,
M. Rizzolio, R. Rynberg, B. P. Scott,
J. Breitenbucher, S. R. Chaplan
10:40 500. Discovery of PF-04457845, an irreversible
FAAH inhibitor with exquisite
selectivity. D. S. Johnson
11:20 501. Discovery and development of
inhibitors of fatty acid amide hydrolase
(FAAH). D. L. Boger
Targeting Gram-Negative Pathogens
Sponsored by COMP, Cosponsored by CINF
and MEDI
THURSDAY AFTERNOON
Section A
Boston Convention & Exhibition Center
Room 259A/B
General Oral Session
J. Zablocki, Organizer, Presiding
1:30 502. Nicotinamide derivatives as novel,
potent and orally active mGlu5 receptor
antagonists. R. Glatthar, I. Vranesic,
C. Spanka, D. Orain, S. Desrayaud,
M. Fendt, D. Hoyer, Y. P. Auberson,
K. H. McAllister, M. T. Wyss, A. Buck
1:45 503. Development of long term manufacturing
process for MK-0633 (Setileuton).
H. Li, J. Balsells-padros,
G. Humphrey, C. Chen, B. Cohen,
D. J. Kumke, F. Gosselin, C. Nadeau,
S. Dolman, P. O’Shea
2:00 504. Apolipoprotein B-100: A 3-iodothyronamine
(T1AM) binding protein.
G. Roy, T. Scanlan
2:15 505. Resorcinol-class HSP90 inhibitors
for oral treatment in oncology.
H. Eggenweiler, C. Sirrenberg,
H. Buchstaller, M. Wolf, U. Grädler,
J. März, D. Musil, E. Hoppe,
A. Zimmermann, C. Amendt,
H. Schwartz, J. Bomke, A. Wegener,
T. Mohr, H. Bauer, M. Brändle,
M. Braendle, J. Gleitz, N. Huebler,
T. Selzer
2:30 506. Design and synthesis of potent,
dual action p53/MDM2/MDMX antagonists
for the treatment of cancer.
K. Wang, W. Wang, G. M. Popowicz,
A. Czarna, S. Wolf, D. Alexander,
T. A. Holak
2:45 507. Synthesis and evaluation of hadacidin
analogs. N. Tibrewal, G. I. Elliott
3:00 508. Trypanosomal target of rapamycin:
Repurposing of mammalian TOR inhibitors
for neglected disease drug discovery.
C. E. Hubbard, S. M. Beverley,
R. Diaz, L. Madeira da Silva, M. Navarro,
M. J. Ondrechen, Z. Wang, M. P. Pollastri
3:15 509. Discovery of a fluorescent cyclindependant
kinase inhibitor with potent
antiproliferative activity in human breast
cancer cells. V. M. Yenugonda,
T. B. Deb, S. C. Grindrod,
S. Dakshanamurthy, Y. Yang, M. Paige,
M. L. Brown
3:30 510. Discovery of phenoxy thiophene
sulfonamides as new potentiators of
Nerve Growth Factor (NGF)-induced neurite
outgrowth. A. L. Williams,
S. R. Dandepally, N. Gilyazova,
S. M. Witherspoon, G. Ibeanu
3:45 511. Synthesis, SAR and biological
evaluation of novel benzimidazoles targeting
FtsZ for drug discovery of efficacious
antitubercular agents. K. Kumar,
D. Awasthi, B. Ruzsicska, P. J. Tonge,
R. A. Slayden, I. Ojima
4:00 512. De novo purine biosynthesis as a
novel antibiotic target. H. Paritala,
J. B. Thoden, H. M. Holden,
S. M. Firestine
4:15 513. Imaging of amyloid beta species
by using spectral unmixing with a “smart”
fluorescence probe. C. Ran,A.Moore
4:30 514. New potential drug against obesity:
Design and synthesis of ghrelin receptor
antagonists. A. Blayo, J. Martinez,
J. Fehrentz
4:45 515. Inhibitors of protein-amyloid interactions
protect cells from �-amyloid-induced
oxidative stress and toxicity.
L. K. Habib, J. Yang
Targeting Gram-Negative Pathogens
Sponsored by COMP, Cosponsored by CINF
and MEDI
The official technical program
for the 240th National Meeting
is available at:
www.acs.org/boston2010
MEDI
TECH–81